S80390 |
SB 202190 |
源叶(MedMol) | 99% |
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- 产品描述: SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits. SB202190 induces autophagy
- 靶点: p38α:50 nM (IC50);p38β2:100 nM (IC50);Apoptosis;p38MAPK;Autophagy
- 体外研究:
SB 202190 (0-10 μM; 0-72 hours) attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner. SB 202190 strongly inhibited colony formation and anchorage-independent growth (10 μM for 7–10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480). In RKO, CACO2 and SW480 cells, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling
- 体内研究:
SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) shows inhibition of tumor cell survival and tumor growth. Animal Model: 4-week-old female BALB/c nude mice (bearing SW480 and RKO xenograft tumors) Dosage: 5 mg/kg Administration: Intraperitoneal injection; daily for 10-12 days Result: Inhibition of tumor cell survival and tumor growth.
- 参考文献:
1. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. 2. Nemoto S, et al. Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20. 3. Grossi V, et al. Bay 43-9006 inhibits p38α activity in colorectal cancer cells and synergizes with the DFG-in inhibitor SB202190 to increase apoptotic response. Cancer Biol Ther. 2012 Dec;13(14):1471-81. 4. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798. 5. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56.
- 溶解性: soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.018 ml 15.09 ml 30.18 ml 5 mM 0.604 ml 3.018 ml 6.036 ml 10 mM 0.302 ml 1.509 ml 3.018 ml 50 mM 0.06 ml 0.302 ml 0.604 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)